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Submit ReviewXanthohumol is a p97 ATPase (VCP) inhibitor. Binds to the N domain of p97, impairing autophagosome function and maturation. Inhibits proliferation and induces apoptosis in a variety of human cancer cell lines. Also inhibits DGAT in rat liver microsomes (IC50 = 50.3 μM).
Xanthohumol is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 354.4 |
Formula | C21H22O5 |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 6754-58-1 |
PubChem ID | 639665 |
InChI Key | ORXQGKIUCDPEAJ-YRNVUSSQSA-N |
Smiles | OC1=C(C(/C=C/C2=CC=C(O)C=C2)=O)C(OC)=CC(O)=C1C/C=C(C)/C |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 35.44 | 100 | |
ethanol | 35.44 | 100 |
The following data is based on the product molecular weight 354.4. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.82 mL | 14.11 mL | 28.22 mL |
5 mM | 0.56 mL | 2.82 mL | 5.64 mL |
10 mM | 0.28 mL | 1.41 mL | 2.82 mL |
50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
References are publications that support the biological activity of the product.
Sasazawa et al (2012) Xanthohumol impairs autophagosome maturation through direct inhibition of valosin-containing protein. ACS Chem.Biol. 7 892 PMID: 22360440
Tabata et al (1997) Xanthohumols, diacylglycerol acyltransferase inhibitors, from Humulus lupulus. Phytochemistry 46 683 PMID: 9366096
Inokoshi et al (2009) Expression of two human acyl-CoA:diacylglycerol acyltransferase isozymes in yeast and selectivity of microbial inhibitors toward the isozymes. J.Antibiot.(Tokyo) 62 51 PMID: 19132064
If you know of a relevant reference for Xanthohumol, please let us know.
Keywords: Xanthohumol, Xanthohumol supplier, valosin-containing, protein, VCP, transitional, endoplasmic, reticulum, ATPase, TER, inhibitors, autophagosome, autophagy, apoptosis, inhibits, Autophagy, Diacylglycerol, O-Acyltransferase, Other, ER, stress/UPR, p97, 4686, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Xanthohumol include:
Muthusamy et al (2017) Antiproliferative and apoptotic effects of xanthohumol in cholangiocarcinoma. Oncotarget 8 88069-88078 PMID: 29152142
den Brok et al (2016) Saponin-based adjuvants induce cross-presentation in dendritic cells by intracellular lipid body formation Nature Communications 7 13324 PMID: 27819292
Do you know of a great paper that uses Xanthohumol from Tocris? Please let us know.
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This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.